US 12,144,811 B2
Combination of a 4-pyrimidinesulfamide derivative with an SGLT-2 inhibitor for the treatment of endothelin related diseases
Marc Bellet, Allschwil (CH); Marc Iglarz, Allschwil (CH); and Martin Bolli, Allschwil (CH)
Assigned to IDORSIA PHARMACEUTICALS LTD, Allschwil (CH)
Appl. No. 16/768,604
Filed by IDORSIA PHARMACEUTICALS LTD, Allschwil (CH)
PCT Filed Nov. 29, 2018, PCT No. PCT/EP2018/082947
§ 371(c)(1), (2) Date May 29, 2020,
PCT Pub. No. WO2019/106066, PCT Pub. Date Jun. 6, 2019.
Claims priority of application No. PCT/EP2017/081050 (WO), filed on Nov. 30, 2017.
Prior Publication US 2021/0169881 A1, Jun. 10, 2021
Int. Cl. A61K 31/506 (2006.01); A61K 9/00 (2006.01); A61K 9/20 (2006.01); A61K 31/7004 (2006.01); A61K 31/7048 (2006.01); A61P 3/10 (2006.01); A61P 7/00 (2006.01); A61P 13/12 (2006.01)
CPC A61K 31/506 (2013.01) [A61K 9/0053 (2013.01); A61K 9/2018 (2013.01); A61K 9/2054 (2013.01); A61K 31/7004 (2013.01); A61K 31/7048 (2013.01); A61P 3/10 (2018.01); A61P 7/00 (2018.01); A61P 13/12 (2018.01)] 31 Claims
OG exemplary drawing
 
1. A pharmaceutical composition containing, as active principles, aprocitentan, or a pharmaceutically acceptable salt thereof, in combination with an SGLT-2 inhibitor, which is atigliflozin, bexagliflozin, canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, henagliflozin, ipragliflozin, luseogliflozin, remogliflozin, sotagliflozin, or tofogliflozin, or a pharmaceutically acceptable salt thereof, as well as at least one pharmaceutically acceptable excipient;
wherein said composition comprises aprocitentan in crystalline form, wherein said crystalline form is characterized by the presence of peaks in the X-ray powder diffraction diagram at the following angles of refraction 2θ: 17.8°, 18.6°, 20.0°, 23.2° and 23.5°; wherein said X-ray powder diffraction diagram is obtained by using combined Cu Kα1 and Kα2 radiation, without Kα2 stripping; and the accuracy of the 2θ values is in the range of 2θ+/−0.2°.